Patent classifications
C07H5/06
HEPARIN-BINDING CATIONIC PEPTIDE SELF-ASSEMBLING PEPTIDE AMPHIPHILES USEFUL AGAINST DRUG-RESISTANT BACTERIA
Disclosed are peptides comprising an amphiphilic backbone and a cationic heparin-binding motif peptide. The peptides can be used in methods of antimicrobial treatment.
USE OF NOCARDIA RUBRA CELL WALL SKELETON IN TREATMENT OF THERMAL INJURY
Provided is the use of a Nocardia rubra cell wall skeleton in the preparation of a drug for treating thermal injury.
USE OF NOCARDIA RUBRA CELL WALL SKELETON IN TREATMENT OF THERMAL INJURY
Provided is the use of a Nocardia rubra cell wall skeleton in the preparation of a drug for treating thermal injury.
Fluorinated N-acetyl glucosamine analogs and xylose derivatives
The present disclosure relates to analogs of N-acetyl glucosamine fluorinated at 4- and/or 6-position(s) and derivatives of xylose at anomeric position for the treatment of a neurological disease, inflammation, cancer and a central nervous system injury.
Fluorinated N-acetyl glucosamine analogs and xylose derivatives
The present disclosure relates to analogs of N-acetyl glucosamine fluorinated at 4- and/or 6-position(s) and derivatives of xylose at anomeric position for the treatment of a neurological disease, inflammation, cancer and a central nervous system injury.
Diglycosylated benzophenoxazine photosensitizer and preparation method and use thereof
Disclosed are a diglycosylated benzophenoxazine photosensitizer, and a preparation method and use thereof. The present invention greatly improves the enriched concentration of the photosensitizer in tumor cells by taking full advantage of the enhanced uptake and enhanced glycolysis of carbohydrates by tumor cells and the glycosylation of a selenium-containing benzophenoxazine compound, thereby improving the targeting of a diglycosylated benzophenoxazine photosensitizer involved in the present invention in the treatment of cutaneous tumors and also significantly decreasing the toxic and side effects of the photodynamic therapy. The present invention can efficiently and rapidly inhibit the proliferation of cells of cutaneous squamous cell carcinoma and essentially cause no damage to normal cells.
Methods for the preparation of ribosides
- Steven Donald Axt ,
- Pavel Robertovich Badalov ,
- Katrien Brak ,
- Silvio Campagna ,
- Andrei Chtchemelinine ,
- Edward Doerffler ,
- Morin Mae Frick ,
- Detian Gao ,
- Lars V. Heumann ,
- Brittanie Hoang ,
- Willard Lew ,
- Robert Ronald MILBURN ,
- Sean Timothy Neville ,
- Bruce Ross ,
- Erik Rueden ,
- Robert William Scott ,
- Dustin Siegel ,
- Andrew C. Stevens ,
- Clarissa Tadeus ,
- Tiago Vieira ,
- Andrew W. Waltman ,
- Xianghong Wang ,
- Mark Charles Whitcomb ,
- Lydia Wolfe ,
- Chia-Yun Yu
Provided are methods of preparing compounds and pharmaceutical compositions comprising a compound Formula VIII for treating Filoviridae virus infections. In one aspect, the compound of Formula VIII is formed from a reaction mixture comprising the compound of Formula IX, the compound of Formula X, a coupling agent such as magnesium chloride and a non-nucleophilic base such as diisopropylethylamine. The compound of Formula IX can be formed from a compound of Formula V and a cyanating agent. The compound of Formula V can be synthesized from a reaction mixture comprising a deprotonating agent such as phenylmagnesium chloride; a silylating agent such as chlorotrimethylsilane; a coupling agent such as isopropylmagnesium chloride, an additive such as LaCl.sub.3-2LiCl, LaCl.sub.3, CeCl.sub.3, NdCl.sub.3, or YCl.sub.3; a compound of Formula VI; and 7-iodopyrrolo[2,1-f][1,2,4]triazin-4-amine. The compounds, compositions, and methods provided are particularly useful for the treatment of Marburg virus, Ebola virus and Cueva virus infections.
3-DEOXY-2-KETOALDONIC ACID NITROGEN-CONTAINING DERIVATIVE, PREPARATION METHOD THEREOF, AND USE THEREOF
The invention relates to a compound represented by general Formula I, a stereoisomer thereof, a pharmaceutically acceptable salt thereof, a pharmaceutically acceptable ester thereof, a pharmaceutically acceptable hydrate thereof or pharmaceutically acceptable solvate thereof and the invention also relates to a pharmaceutical composition comprising the compound, and a preparation method for the compound and a use of the compound.
##STR00001##
3-DEOXY-2-KETOALDONIC ACID NITROGEN-CONTAINING DERIVATIVE, PREPARATION METHOD THEREOF, AND USE THEREOF
The invention relates to a compound represented by general Formula I, a stereoisomer thereof, a pharmaceutically acceptable salt thereof, a pharmaceutically acceptable ester thereof, a pharmaceutically acceptable hydrate thereof or pharmaceutically acceptable solvate thereof and the invention also relates to a pharmaceutical composition comprising the compound, and a preparation method for the compound and a use of the compound.
##STR00001##
Process for the preparation of GalNAc oligonucleotide conjugates
The invention comprises a process for the preparation of GalNAc oligonucleotide conjugates which comprises the coupling of a GalNAc cluster compound of the formula ##STR00001##
or corresponding salts, enantiomers and/or a stereoisomer thereof, with an oligonucleotide in the presence of an O-dicarboximidouronium salt as coupling agent.